Erythrocyte Partitioning Profile of Isosteviol in Human and Rat Blood.

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ID: 81117
2019
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Abstract
Isosteviol is a synthetic derivative of steviol glycosides with promising pharmacological properties and might find future use as a cardioprotective agent.A simple LC-MS/MS technique was developed and validated for the bioanalysis of isosteviol in plasma and erythrocytes. This method was subsequently utilized for the in vitro assessment of isosteviol's partitioning into blood compartments of humans and rats.Fresh blood samples from healthy humans and Wistar rats were equilibrated with 1, 10, and 30 µM isosteviol at 37 °C in a shaking dry-bath. The levels of isosteviol in plasma and erythrocytes partitions were determined in these samples, after separation, at intervals over a 60-minute period. The data derived was used to estimate erythrocyte-to-plasma and blood-to-plasma coefficients.Mean erythrocyte-to-plasma partition coefficients (SD) after 60 minutes of equilibration were observed to be 0.039 (0.002) and 0.040 (0.003) in humans and rats, respectively. Derived values for the blood-to-plasma ratio (SD) were 0.576 (0.001) in humans and 0.543 (0.007) in rats, whereas plasma component binding was estimated to be more than 96%.The findings suggest that isosteviol preferentially partitions into plasma compartments in humans and rats. The significance of this profile for the efficacy, tissue uptake, and retention of isosteviol will have to be further studied.
Reference Key
adehin2019erythrocytecurrent Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Adehin, Ayorinde;Tan, Keai Sinn;Tan, Wen;
Journal current therapeutic research, clinical and experimental
Year 2019
DOI
10.1016/j.curtheres.2019.06.003
URL
Keywords
neuroprotection steviol glycosides erythrocytes isosteviol cardioprotective agent partitioning ratio

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